Sialyltransferase Inhibitor

ST6GAL1-IN-1 is an orally active selective ST6GAL1 inhibitor (IC₅₀ = 20 μM). ST6GAL1-IN-1 exhibits high antimetastatic potential, effectively inhibiting the migration of MDA-MB-231 cells at noncytotoxic concentrations. ST6GAL1-IN-1 can disrupt integrin sialylation in MDA-MB-231 cells. ST6GAL1-IN-1 inhibits tumor angiogenesis and cancer metastasis via the Integrin/VEGFR2-mediated signaling pathway. ST6GAL1-IN-1 effectively suppresses both tumor growth and cancer metastasis on the MDA-MB-231 xenograft model. ST6GAL1-IN-1 can be used for the study of Triple-negative breast cancer (TNBC).

SPP-002 is a ST6GAL1 inhibitor with a human IC₅₀ of 16.7 μM. SPP-002 selectively inhibits N-glycan sialylation over O-glycan sialylation and binds strongly to the enzyme active site. SPP-002 suppresses expression of signaling proteins in the integrin/FAK/paxillin pathway. SPP-002 can be used for the research of triple negative breast cancer metastasis.

IAN-15B has high selectivity and potent ST6GAL1 inhibitors (IC₅₀ = 3.3 μM). IAN-15B has significant anti migratory and anti angiogenic effects. IAN-15B can be used in the research of cancer such as breast cancer.

SPP-037 is an orally active and selective inhibitor of ST6GAL1 (IC₅₀ = 3.59 μM). SPP-037 inhibits integrin α2,6-sialylation and integrin-FAK-paxillin pathway. SPP-037 inhibits cancer cell proliferation, migration and exhibits antiangiogenic activity. SPP-037 has anti-tumor activity in MDA-MB-231 xenograft mouse model. SPP-037 can be used for the research of triple-negative breast cancer.

EBU-141 is a human monoclonal antibody (mAb) targeting CD75/ST6GAL1. EBU-141 can be used in B-cell lymphoma and multiple myeloma research.